Pharmacodynamics anadrol 50 is highly selective nonsteroidal aromatase inhibitor – an enzyme, whereby in postmenopausal women androstenedione in peripheral tissues is converted into estrone and then to estradiol. Reduced levels of circulating estradiol in breast cancer patients has a therapeutic effect. In postmenopausal women, anadrol 50 at a daily dose of 1 mg estradiol levels causes a decrease of 80%.
anadrol 50 has no progestogenic, androgenic and estrogenic activity. anadrol 50 at daily doses up to 10 mg had no effect on the secretion of aldosterone and cortisol, therefore the application is not required substitution anadrol 50 corticosteroids.
Absorption anadrol 50 prompt, the maximum plasma concentration is reached within 2 hours after ingestion (fasting). Food slightly decreases the rate of absorption, but not its extent and does not result in a clinically significant effect on the equilibrium concentration of drug in blood plasma after a single reception daily dose of anadrol 50. After 7-day dosing is achieved approximately 90 – 95% of the equilibrium concentration of anadrol 50 in plasma. Recorded anadrol 50 pharmacokinetic parameters depending on the time or dose not. The pharmacokinetics of anadrol 50 is independent of age in postmenopausal women. Contact with blood plasma proteins -. 40%
Anastrazole displayed slowly, half-life from plasma is 40-50 hours. Extensively metabolized in postmenopausal women. Less than 10% of the dose is excreted in the urine unchanged within 72 hours after ingestion. Metabolism performed during N-dealkylation, hydroxylation and glucuronidation. Metabolites are excreted mainly by the kidneys. Triazole major metabolite determined in blood plasma does not possess pharmacological activity.
Total clearance after oral administration of anadrol 50 in cirrhosis or renal dysfunction is not changed.
• Adjuvant treatment of early breast cancer, hormone receptor-positive postmenopausal women, including after adjuvant tamoxifen therapy for 2-3 years.
• First-line treatment of locally advanced or metastatic breast cancer with positive or unknown hormone receptor in postmenopausal women.
• The second-line treatment of advanced breast cancer progressing after treatment with tamoxifen in postmenopausal women.
– Hypersensitivity to anadrol 50 or other components of the preparation.
– In premenopausal women.
– Severe hepatic impairment (safety and efficacy not established).
– Concomitant therapy with tamoxifen.
– Pregnancy and lactation.
– Children’s age (safety and efficacy in children not installed)
Precautions : lactase deficiency, galactose intolerance, glucose-galactose malabsorption (lactose contained in the dosage form of the drug).
Dosing and Administration
Inside. Swallow the tablet whole with water. It is recommended to take the drug at the same time, regardless of the meal. Adults, including the elderly : 1 mg orally 1 time a day for a long time. As an adjuvant therapy, the recommended duration of treatment – 5 years. If signs of progression of the disease taking the drug should be discontinued. Renal function : a dose adjustment in patients with impaired renal function is not required. Violations of the liver : a dose adjustment in patients with mild to moderate impaired liver function is not required.
The frequency of adverse reactions listed below was determined according to the following criteria: very often (at least 1.10); frequently (more than 1/100 of less than 1/10.); sometimes (more than 1/1000 of less than 1/100.); rarely (over 1/10000, 1/1000 less); very rare (less than 1/10000), including isolated reports. On the part of the vessels: very often – “tides” of blood to the face. On the part of the musculoskeletal and connective tissue disorders: very often – arthralgia / joint stiffness, arthritis; often – bone pain, myalgia; infrequently – trigterny finger. From the genital and breast cancer: often – dryness of the vaginal mucosa, vaginal bleeding (mainly in the first weeks after the cancellation or change of previous hormonal therapy anadrol 50). Skin and subcutaneous tissue disorders: very common – skin rash; often – thinning hair, alopecia, allergic reactions; rarely – urticaria; rarely – erythema multiforme, anaphylactoid reactions, cutaneous vasculitis (including isolated cases of purpura (Henoch-Henoch syndrome)), very rarely – Stevens-Johnson Syndrome, angioedema. On the part of the gastrointestinal tract: often – nausea; often – diarrhea, vomiting. Liver and biliary tract: often – increasing the activity of alkaline phosphatase, alanine aminotransferase, aspartate aminotransferase; rarely – increased activity of gamma glutamintransferazy and bilirubin, hepatitis. From the nervous system: very often – headache; often – drowsiness, carpal tunnel syndrome (mainly seen in patients with risk factors for the patients of the disease), sensory disturbances (including paraesthesia, loss or distortion of taste sensation). On the part of metabolism and nutrition: often – anorexia, hypercholesterolemia; seldom – hypercalcemia (with / without increasing paratgormoia concentration). The drug can cause a reduction in bone mineral density due to lower concentrations of circulating estradiol, thereby increasing the risk of osteoporosis and bone fractures. General disorders: very often – asthenia, mild or moderate in severity. Adverse events reported in clinical trials are not associated with taking anadrol 50: anemia, constipation, indigestion, back pain, abdominal pain, increased blood pressure, weight gain, depression, insomnia, dizziness, anxiety, paresthesia.
We describe the individual clinical cases of accidental overdose. A single dose of anadrol 50, which could lead to the symptoms, life-threatening, has not been established.
The specific antidote does not exist; in the case of overdose, treatment should be symptomatic. It is possible to induce vomiting if the patient is conscious. Dialysis can be performed. Recommended general supportive therapy, monitoring patients and control the function of vital organs and systems.
Interaction with other drugs
Clinically significant drug interactions when taking anadrol 50 in conjunction with other commonly prescribed drugs available.
At the moment, there are no data on the use of anadrol 50 in combination with other anticancer drugs.
Studies on drug interactions with phenazone and cimetidine indicate that the combined use of anadrol 50 with other drugs is unlikely to result in clinically significant drug interactions mediated by cytochrome P450.
Preparations containing estrogens reduce the pharmacological effect of anadrol 50, and therefore, they should not be administered concurrently with anadrol 50.
it should appoint tamoxifen concurrently with anadrol 50 because it can weaken the pharmacological action of the latter.
The safety and efficacy of anadrol 50 in children has not been established.
Women with retseptorootritsatelnoy tumor estrogen efficacy of anadrol 50 has not been demonstrated, except in cases where there was a previous positive clinical response to tamoxifen.
In case of doubt in the hormonal status of the patient menopause must be confirmed by the definition of sex hormones serum.
There are no data on the use of anadrol 50 in patients with severe liver dysfunction.
In the case of persistent uterine bleeding in patients receiving anadrol 50 need advice and supervision of the gynecologist.
preparations containing estrogens should not be administered concurrently with anadrol 50, as these drugs will reverse the its pharmacological effect.
by reducing the level of circulating estradiol, anadrol 50 can cause a reduction in bone mineral density
in patients with osteoporosis or have risk of developing osteoporosis, bone mineral density should be assessed by densitometry (eg, DEXA scan) at the beginning of treatment and in the dynamics. If necessary, must be initiated by the treatment or prevention of osteoporosis under the close supervision of a physician.
No data on the concomitant use of anadrol 50 and preparations analog of luteinizing hormone-releasing hormone (LHRH).
It is unknown whether anadrol 50 results improves treatment when used in conjunction with chemotherapy.
The efficacy and safety at the same time use of tamoxifen, regardless of hormone receptor status comparable with those using a tamoxifen.
Some side effects of anadrol 50, such as fatigue and drowsiness, may adversely affect the ability to perform potentially hazardous activities that require high concentration and speed of psychomotor reactions. In this connection, it is recommended with the appearance of these symptoms to be careful in the management of vehicles and mechanisms.